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Merck

SML1867

Sigma-Aldrich

NVS-PAK1-1

≥98% (HPLC)

Sinónimos:

(S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide

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About This Item

Fórmula empírica (notación de Hill):
C23H25ClF3N5O
Número de CAS:
Peso molecular:
479.93
UNSPSC Code:
41106609
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 30 mg/mL, clear

storage temp.

2-8°C

SMILES string

FC(F)CN1C2=C(C=C(Cl)C=C2)C(N[C@H]3CCN(C(NC(C)C)=O)C3)=NC4=C1C=CC(F)=C4

Biochem/physiol Actions

NVS-PAK1-1 is a potent allosteric inhibitor of p21-activated kinase PAK1, a serine-threonine kinase that is upregulated in many cancers. NVS-PAK1-1 has an IC50 value of 5 nM for dephoshorylated PAK1 and 6 nM for phosphorylated PAK1 in an in vitro dephosphorylation assay. NVS-PAK1-1 showed good selectivity against 442 other kinases including PAK2. NVS-PAK1-1 has generally good physicochemical properties, but was metabolized by rat liver microsomes, so may not be useful for in vivo work. For full characterization details, please visit the NVS-PAK1-1 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc

Features and Benefits

NVS-PAK1-1 is a chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC chemical probes, visit sigma.com/SGC
This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificados de análisis (COA)

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